Bcr-Abl

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S1021	Dasatinib	<1 mg/mL	98 mg/mL	<1 mg/mL
S1026	Imatinib Mesylate (STI571)	118 mg/mL	118 mg/mL	<1 mg/mL
S1490	Ponatinib (AP24534)	<1 mg/mL	30 mg/mL	<1 mg/mL
S1033	Nilotinib (AMN-107)	<1 mg/mL	27 mg/mL	<1 mg/mL
S1107	Danusertib (PHA-739358)	<1 mg/mL	95 mg/mL	<1 mg/mL
S5254	Dasatinib hydrochloride	-1 mg/mL	100 mg/mL	-1 mg/mL
S5205	Nilotinib hydrochloride	-1 mg/mL	100 mg/mL	-1 mg/mL
S8555	Asciminib (ABL001)	-1 mg/mL	89 mg/mL	89 mg/mL
S3609	Berbamine (dihydrochloride)	100 mg/mL	100 mg/mL	<1 mg/mL
S1134	AT9283	<1 mg/mL	76 mg/mL	38 mg/mL
S2243	Degrasyn (WP1130)	<1 mg/mL	77 mg/mL	18 mg/mL
S1369	Bafetinib (INNO-406)	<1 mg/mL	100 mg/mL	<1 mg/mL
S2158	KW-2449	<1 mg/mL	67 mg/mL	67 mg/mL
S2202	NVP-BHG712	<1 mg/mL	101 mg/mL	3 mg/mL
S2622	PP121	<1 mg/mL	64 mg/mL	2 mg/mL
S2634	Rebastinib (DCC-2036)	<1 mg/mL	111 mg/mL	16 mg/mL
S7194	GZD824 Dimesylate	100 mg/mL	100 mg/mL	<1 mg/mL
S2899	GNF-2	<1 mg/mL	74 mg/mL	<1 mg/mL
S7782	Dasatinib Monohydrate	<1 mg/mL	21 mg/mL	<1 mg/mL
S8134	Radotinib	<1 mg/mL	100 mg/mL	<1 mg/mL
S7269	PD173955	<1 mg/mL	15 mg/mL	<1 mg/mL
S8140	GNF-7	<1 mg/mL	20 mg/mL	<1 mg/mL
S7526	GNF-5	<1 mg/mL	83 mg/mL	20 mg/mL

特异性亚型抑制剂

Abl Selective

Bcr-Abl抑制剂（23）
新Bcr-Abl产品

产品目录	产品描述	文献引用	实验数据
S1021	Dasatinib Dasatinib是一种新型有效的多靶点抑制剂，作用于Abl，Src和 c-Kit，在无细胞试验中IC50分别为 <1 nM，0.8 nM 和 79 nM。	Nature, 2017, 543(7647):728-732 Cancer Discov, 2016, 6(7):727-39 Cancer Discov, 2011, 1(7):608-25	Antitumor activity (A)and body weight (B) relationship for BLU-285 and dasatinib in a P815 KIT D814Y mastocytoma allograft model.
S1026	Imatinib Mesylate (STI571) Imatinib Mesylate (STI571)是一种口服生物有效的Imatinib甲磺酸盐，是一种多靶点抑制剂，作用于v-Abl，c-Kit和PDGFR，在无细胞和细胞试验中，IC50分别为0.6 μM，0.1 μM 和0.1 μM。	Cell Stem Cell, 2012, 10(2):210-7 Cancer Cell, 2014, 26(6):840-50 Sci Transl Med, 2014, 6(261):261ra152	THOC5 phospho-Y225 levels were assessed in the populations shown by flow cytometry following 24 h treatment with 5 μM imatinib, 150 nM dasatinib or 5 μM nilotinib. Results are displayed as mean fluorescence intensity (n= 4) ±s.e.m.
S1490	Ponatinib (AP24534) Ponatinib (AP24534)是一种新型有效的多靶点抑制剂，在无细胞试验中作用于Abl，PDGFRα，VEGFR2，FGFR1和Src，IC50分别为0.37 nM，1.1 nM，1.5 nM，2.2 nM和5.4 nM。	Nature, 2015, 10.1038/nature14329 Cancer Discov, 2016, 6(7):727-39 Cancer Cell, 2012, 22(5):656-67	RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT.
S1033	Nilotinib (AMN-107) Nilotinib (AMN-107)是一种特异性BCR-ABL抑制剂，在小鼠骨髓祖细胞中IC50低于30 nM。	Nature, 2016, 534(7607):341-6 Nat Commun, 2015, 6:7002 Cell Death Dis, 2015, 6:e1767	Ba/F3-p210^T315I cells were treated with indicated concentrations of nilotinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05.
S1107	Danusertib (PHA-739358) Danusertib (PHA-739358)是一种Aurora kinase抑制剂，作用于Aurora A/B/C，无细胞试验中IC50为13 nM/79 nM/61 nM，适度有效作用于Abl，TrkA，c-RET和FGFR1，对Lck，VEGFR2/3，c-Kit，CDK2等作用效果稍弱。Phase 2。	Leukemia, 2018, 10.1038/s41375-018-0102-4 Cancer Res, 2014, 74(20):5878-90 Cancer Res, 2013, 73(20):6310-22	c, Upper panel: viable cell number of FLT3-ITD-positive AML patient samples incubated with vandetanib, danusertib, or DMSO for 7 days in methylcellulose. The mean ± SD of duplicates is shown. Lower panel: viability and proliferation of mutant FLT3-positive AML cell lines and one AML patient sample treated with vandetanib and crenolanib alone or in combination for 3 days. The calculated additive effects of both inhibitors according to the Bliss Independence model are indicated by the dashed lines. The mean ± SD of four (cell lines) or two (patient sample) independent experiments is shown. P-values were calculated using one-way ANOVA followed by Dunnett’s test for multiple comparisons. P ≤ 0.05; P ≤ 0.01; **P ≤ 0.001.
S5254^New	Dasatinib hydrochloride Dasatinib hydrochloride is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.
S5205^New	Nilotinib hydrochloride Nilotinib hydrochloride is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
S8555^New	Asciminib (ABL001) Asciminib(ABL001)是一种有效的、选择性的ABL1变构抑制剂，Kd值为0.5-0.8 nM，与ABL1的十四酰口袋结合。
S3609^New	Berbamine (dihydrochloride) Berbamine (BBM)是一种从中草药黄芦木中分离而来的双苄基异喹啉类天然产物。它是bcr/abl的新型抑制剂，具有有效的抗白血病活性，是NF-κB的抑制剂。
S1134	AT9283 AT9283是一种有效的JAK2/3抑制剂，无细胞试验中IC50为1.2 nM/1.1 nM；对Aurora A/B，Abl(T315I)也有效。Phase 2。	Cell Stem Cell, 2012, 11(2):179-94 Cancer Res, 2013, 73(20):6310-22 Cancer Lett, 2013, 341(2):224-30	HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
S2243	Degrasyn (WP1130) Degrasyn (WP1130)是一种选择性deubiquitinase (DUB: USP5，UCH-L1，USP9x，USP14，和 UCH37)抑制剂，对Bcr/Abl也有抑制作用，也是一种JAK2传感器(不影响20S蛋白酶体)和转录激活剂(STAT)。	Trends Pharmacol Sci, 2014, 35(4):187-207 Cancer Res, 2016, 76(8):2384-93 Oncogene, 2014, 10.1038/onc.2014.351	HEK-293 cells expressing Strep-CLASPIN were first arrested in S-phase with HU or in mitosis with nocodazole. Cycloheximide was then added to prevent further protein synthesis in the presence or absence of the USP9X inhibitor WP1130 and samples were harvested at the indicated times. A sample from the same cell line uninduced (U) was loaded as control.
S1369	Bafetinib (INNO-406) Bafetinib (INNO-406)是一种有效的，选择性的，双重Bcr-Abl/Lyn双重抑制剂，无细胞试验中IC50为5.8 nM/19 nM，对T315I突变型的磷酸化没有抑制作用，对PDGFR和c-Kit的作用效果较弱。Phase 2。	J Med Chem, 2015, Int Arch Allergy Immunol, 2012, 159(1):15-22 Exp Hematol, 2015, 10.1016/j.exphem.2015.11.009	(A) The effect of bafetinib at 3 μM on the expression levels of ABCB1 in SW620/Ad300 cells for 24, 48 and 72 h. (B) The effect of bafetinib at 3 μM on the expression level of ABCG2 in NCI-H460/MX20 cells for 24, 48 and 72 h. Equal amounts of total cell lysate were used for each sample. The effect of bafetinib at 3 μM on the subcellular localization of ABCB1 in ABCB1-overexpressing (C) SW620/Ad300 cells and (D) HEK/ABCB1 cells for 24, 48 and 72 h. The effect of bafetinib at 3 μM on the subcellular localization of ABCG2 in ABCG2-overexpressing (E) NCI-H460/MX20 cells and (F) HEK/ABCG2-R482 cells. Scale bar, 10 μm. PI (propidium Iodide, red) counterstains the nuclei.
S2158	KW-2449 KW-2449是一种多靶点抑制剂，最有效作用于Flt3，IC50为6.6 nM，作用于Flt3， Bcr-Abl和Aurora A适度有效；对PDGFRβ， IGF-1R， EGFR没有抑制效果。Phase 1。		Western blot analysis of p-histone and histone. 0-10μM KW2449 was added.
S2202	NVP-BHG712 NVP-BHG712是一种特异性的EphB4抑制剂，ED50为25 nM，区别于对VEGFR和EphB4的抑制，对c-Raf， c-Src和c-Abl也具有抑制活性，IC50分别为0.395 μM， 1.266 μM和1.667 μM。	J Pharmacol Sci, 2015, 129(1):65-71 Anticancer Res, 2014, 34(6):2913-8
S2622	PP121 PP121是一种作用于PDGFR， Hck， mTOR， VEGFR2， Src和Abl的多靶点抑制剂，IC50分别为2 nM， 8 nM， 10 nM， 12 nM， 14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。	Biochem Biophys Res Commun, 2015, 465(1):137-44 Int J Clin Exp Pathol, 2013, 6(10):2082-91 Tumour Biol, 2014, 35(9):8659-64	After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PP-121 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.
S2634	Rebastinib (DCC-2036) Rebastinib (DCC-2036)是一种Bcr-Abl抑制剂，作用于Abl1(WT)和Abl1(T315I)，IC50分别为0.8 nM和4 nM，也抑制SRC， LYN， FGR， HCK， KDR， FLT3，和Tie-2，对c-Kit具有低的抑制活性。Phase 1。	Anal Chem, 2013, 85(15):6995-7002 PLoS One, 2013, 8(8): e73059 Exp Hematol, 2015, 10.1016/j.exphem.2015.11.009	BaF3-T674I cells were exposed to the indicated concentrations of DCC-2036, imatinib or sorafenib for 36 h, the phosphorylated PDGFRα and total PDGFRα were analyzed by immunoblotting. Imatinib was used for comparison.
S7194	GZD824 Dimesylate GZD824 Dimesylate是新型口服有效的Bcr-Abl抑制剂，作用于Bcr-Abl(WT)和Bcr-Abl(T315I)，IC50分别为0.34 nM和0.68 nM。	Oncotarget, 2016, 7(48):79842-79853 Oncotarget, 2016, 7(48):79842-79853	B. Western blot analysis of phosphorylated Akt, S6 and CrkL in T-ALL cell lines treated for 4 h with 2 μM Imatinib or Nilotinib or 0.1 μM GZD824. Twenty-five μg of protein were blotted to each lane. β-Actin documented equal lane loading. Imatinib, Nilotinib and GZD824 were abbreviated in IMA, NIL and GZD.
S2899	GNF-2 GNF-2是一种高选择性，非ATP竞争性的Bcr-Abl抑制剂，对Flt3-ITD， Tel-PDGFR， TPR-MET和Tel-JAK1转化的肿瘤细胞没有作用活性。	Oncotarget, 2017, 8(24):38717-38730	Cell viability of K562/IR cells and their parental cell lines after exposure to different concentrations of GNF-2 for 72 h.
S7782	Dasatinib Monohydrate Dasatinib Monohydrate 是一种新型有效的多靶点抑制剂，作用于靶点Abl，Src 和 c-Kit，IC50分别为 <1 nM，0.8 nM 和 79 nM。	Nature, 2016, 534(7607):341-6 Cancer Discov, 2011, 1(7):608-25 Cell Stem Cell, 2012, 10(2):210-7
S8134	Radotinib Radotinib是一种选择性 BCR-ABL1 酪氨酸激酶抑制剂，IC50 为 34 nM，用于治疗慢性髓性白血病。
S7269	PD173955 PD173955 是一种强效的Bcr-Abl抑制剂，IC50为1-2 nM,同时也可抑制Src活性，IC50为22 nM。
S8140	GNF-7 GNF-7是一种有效的II型激酶Bcr-Abl抑制剂，对M351T，T315I，E255 V，G250E，和 c-Abl的IC50分别为 <5 nM，61 nM，122 nM，136 nM，和 133 nM。
S7526	GNF-5 GNF-5 是一种选择性的，变构的Bcr-Abl抑制剂, IC50为220 nM。	Leukemia, 2017, 31(5):1096-1107 Oncotarget, 2017, 8(24):38717-38730	IC50 values for GNF-5-treated Ba/F3 cells expressing BCR-ABL1 or ABL1 1b mutants (a) described to confer ABL001 resistance in BCR-ABL1, (b) identified by mutagenesis screen. after 48 hours. Error bars represent SD of triplicates from three independent experiments. Significance levels in comparison with BCR-ABL1 are indicated (NS, not significant; P<0.05, P<0.01, **P<0.001, two-tailed unpaired t-test).

研究领域

产品类型

Bcr-Abl

信号通路图

研究领域

特异性亚型抑制剂